Target Validation Information
TTD ID	T69912
Target Name	Platelet-activating factor acetylhydrolase (PLA2G7)
Type of Target	Clinical trial
Drug Potency against Target	Darapladib	Drug Info	IC50 = 0.27 nM	[4]
	(E)-(thiophen-2-ylmethylidene)amino benzoate	Drug Info	IC50 = 11200 nM	[1]
	3,4-difluorobenzaldehyde O-benzoyloxime	Drug Info	IC50 = 2000 nM	[2]
	4-fluorobenzaldehyde O-benzoyloxime	Drug Info	IC50 = 4400 nM	[2]
	Benzaldehyde O-benzoyloxime	Drug Info	IC50 = 3800 nM	[2]
Action against Disease Model	Darapladib	Drug Info	Preclinical studies in diabetic-hypercholesterolemic swine (useful for the study of h uMan atherosclerosis mechanisms) demonstrated that darapladib attenuated the progression ofarterial plaques to a higher-risk phenotype by reducing the n uMber of inflammatory macrophages within plaques and dampening T-cell responses.	[3]
References
REF 1	(E)-Phenyl- and -heteroaryl-substituted O-benzoyl-(or acyl)oximes as lipoprotein-associated phospholipase A2 inhibitors. Bioorg Med Chem Lett. 2005 Mar 1;15(5):1525-7.
REF 2	Potent inhibitors of lipoprotein-associated phospholipase A(2): benzaldehyde O-heterocycle-4-carbonyloxime. Bioorg Med Chem Lett. 2006 Nov 1;16(21):5576-9.
REF 3	Darapladib, a reversible lipoprotein-associated phospholipase A2 inhibitor, for the oral treatment of atherosclerosis and coronary artery disease. IDrugs. 2009 Oct;12(10):648-55.
REF 4	Darapladib. Expert Opin Investig Drugs. 2010 Jan;19(1):161-8.

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